[2-氧代-4-(三氟甲基)苯并吡喃-7-基]磷酸二氢酯 | 122018-93-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 中文名称: [2-氧代-4-(三氟甲基)苯并吡喃-7-基]磷酸二氢酯
• 英文名称: 4-Trifluoromethylcoumarin phosphate
• 英文别名: [2-oxo-4-(trifluoromethyl)chromen-7-yl] dihydrogen phosphate
• CAS: 122018-93-3
• 化学式: C₁₀H₆F₃O₆P
• 分子量: 310.12
• InChiKey: ZXSQZYGFCBGKMY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  93.1
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• [EN] SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS<br/>[FR] ACÉTAMIDES HÉTÉROCYCLIQUES SUBSTITUÉS EN TANT QU'AGONISTES DU RÉCEPTEUR OPIOÏDE KAPPA (KOR)
  申请人：REDDYS LAB LTD DR

  公开号：WO2013131408A1

  公开（公告）日：2013-09-12

  The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

  本发明涉及一系列具有通式（I）的取代化合物，包括它们的立体异构体和/或其药用盐，其中R1、R2、R3、R4、R5和R6如本文所定义。本发明还涉及制备这些化合物的方法，包括中间体。本发明的化合物在kappa（κ）阿片受体（KOR）位点上具有有效性。因此，本发明的化合物可用作药物剂，特别是在治疗和/或预防各种中枢神经系统疾病（CNS）方面，包括但不限于急性和慢性疼痛，以及相关疾病，尤其是在中枢神经系统的外周起作用。
• In situ detection of nucleotide variants in high noise samples, and compositions and methods related thereto
  申请人：Advanced Cell Diagnostics, Inc.

  公开号：US11078528B2

  公开（公告）日：2021-08-03

  The invention relates to methods of in situ detection of a nucleic acid variation of a target nucleic acid in a sample, including single nucleotide variations, multi-nucleotide variations or splice sites. The method can comprise the steps of contacting the sample with a probe that detects the nucleic acid variation or splice site and a neighbor probe; contacting the sample with pre-amplifiers that bind to the nucleic acid variation probe or splice site probe and neighbor probe, respectively; contacting the sample with a collaboration amplifier that binds to the pre-amplifiers; and contacting the sample with a label probe system, wherein hybridization of the components forms a signal generating complex (SGC) comprising a target nucleic acid with the nucleic acid variation or splice site, the probes and amplifiers; and detecting in situ signal from the SGC on the sample. The invention also provides samples, tissue slides, and kits relating to detection of nucleic acid variations, including single nucleotide variations, multi-nucleotide variations or splice sites, of a target nucleic acid.

  本发明涉及原位检测样品中目标核酸变异的方法，包括单核苷酸变异、多核苷酸变异或剪接位点。该方法可包括以下步骤：用检测核酸变异或剪接位点的探针和邻接探针接触样品；用分别与核酸变异探针或剪接位点探针和邻接探针结合的前置放大器接触样品；用与前置放大器结合的协作放大器接触样品；将样品与标记探针系统接触，其中各组分杂交形成信号发生复合物（SGC），该复合物由靶核酸与核酸变异或剪接位点、探针和放大器组成；检测样品上 SGC 的原位信号。本发明还提供了与检测核酸变异（包括目标核酸的单核苷酸变异、多核苷酸变异或剪接位点）有关的样品、组织切片和试剂盒。
• Terminal-phosphate-labeled nucleotides and methods of use
  申请人：——

  公开号：US20030077610A1

  公开（公告）日：2003-04-24

  The present invention describes methods of detecting a nucleic acid in a sample, based on the use of terminal-phosphate-labeled nucleotides as substrates for nucleic acid polymerases. The methods provided by this invention utilize a nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogue which has a colorimetric dye, chemiluminescent, or fluorescent moiety, a mass tag or an electrochemical tag attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.

  本发明描述了基于使用末端磷酸标记的核苷酸作为核酸聚合酶底物来检测样品中核酸的方法。本发明提供的方法利用核苷酸多聚磷酸酯、二脱氧核苷酸多聚磷酸酯或脱氧核苷酸多聚磷酸酯类似物，这些核苷酸多聚磷酸酯类似物具有连接到末端磷酸酯上的比色染料、化学发光或荧光分子、质量标签或电化学标签。当核酸聚合酶使用这种类似物作为底物时，磷酸转移的无机多磷酸副产物上就会出现酶活标签。通过磷酸酶裂解磷酰转移的多磷酸产物会导致其上附着的标签发生可检测的变化。当聚合酶检测在磷酸酶存在的情况下进行时，就提供了一种实时监测 DNA 或 RNA 合成和检测目标核酸的便捷方法。
• Single nucleotide amplification and detection by polymerase
  申请人：——

  公开号：US20030096253A1

  公开（公告）日：2003-05-22

  A method of characterizing a nucleic acid sample is provided that includes the steps of: (a) conducting a DNA polymerase reaction that includes the reaction of a template, a non-hydrolyzable primer, at least one terminal phosphate-labeled nucleotide, DNA polymerase, and an enzyme having 3′→5′ exonuclease activity which reaction results in the production of labeled polyphosphate; (b) permitting the labeled polyphosphate to react with a phosphatase to produce a detectable species characteristic of the sample; (c) detecting the detectable species; and (d) characterizing the nucleic acid sample based on the detection.

  提供了一种表征核酸样本的方法，该方法包括以下步骤(a) 进行 DNA 聚合酶反应，该反应包括模板、非水解引物、至少一种末端磷酸盐标记的核苷酸、DNA 聚合酶和具有 3′→5′ 外切酶活性的酶的反应，该反应导致产生标记的聚磷酸盐；(b) 使标记的多聚磷酸盐与磷酸酶反应，产生具有样品特征的可检测物； (c) 检测可检测物；以及 (d) 根据检测结果确定核酸样品的特征。
• Labeled nucleoside polyphosphates
  申请人：——

  公开号：US20030124576A1

  公开（公告）日：2003-07-03

  The present invention describes new compositions of matter in the form of labeled nucleoside polyphosphates with four or more phosphates. In addition compositions of nucleoside polyphosphates with four or more phosphates that are substrates for nucleic acid polymerases with enhanced substrate properties and methods of using these nucleoside polyphosphates for nucleic acid detection, charcterization and quantification are described. The compositions provided by this invention include nucleoside polyphosphate, dideoxynucleoside polyphosphate, or deoxynucleoside polyphosphate analogues which have calorimetric, chemiluminescent, or fluorescent moieties, mass tags or an electrochemical tags attached to the terminal-phosphate. When a nucleic acid polymerase uses this analogue as a substrate, an enzyme-activatable label would be present on the inorganic polyphosphate by-product of phosphoryl transfer. Cleavage of the polyphosphate product of phosphoryl transfer via phosphatase leads to a detectable change in the label attached thereon. When the polymerase assay is performed in the presence of a phosphatase, there is provided a convenient method for real-time monitoring of DNA or RNA synthesis and detection of a target nucleic acid.

  本发明描述了具有四个或更多磷酸盐的标记核苷多磷酸盐形式的新物质组合物。此外，本发明还描述了作为核酸聚合酶底物的具有四个或更多磷酸盐的核苷聚磷酸盐的组合物，这些组合物具有增强的底物特性，以及使用这些核苷聚磷酸盐进行核酸检测、鉴定和定量的方法。本发明提供的组合物包括核苷聚磷酸盐、双脱氧核苷聚磷酸盐或脱氧核苷聚磷酸盐类似物，它们的末端磷酸盐上附有热量测定、化学发光或荧光分子、质量标签或电化学标签。当核酸聚合酶使用这种类似物作为底物时，磷酰转移的无机多磷酸副产物上就会出现酶活标签。通过磷酸酶裂解磷酰转移的多磷酸盐产物会导致其上附着的标签发生可检测的变化。当聚合酶检测在磷酸酶存在的情况下进行时，就提供了一种实时监测 DNA 或 RNA 合成和检测目标核酸的便捷方法。